(19)
(11) EP 0 443 573 A3

(12) EUROPEAN PATENT APPLICATION

(88) Date of publication A3:
10.06.1992 Bulletin 1992/24

(43) Date of publication A2:
28.08.1991 Bulletin 1991/35

(21) Application number: 91102531.0

(22) Date of filing: 21.02.1991
(51) International Patent Classification (IPC)5C07K 5/02, A61K 37/64, A61K 37/02, C07K 1/00
(84) Designated Contracting States:
AT BE CH DE DK ES FR GB GR IT LI LU NL SE

(30) Priority: 23.02.1990 US 484135

(71) Applicant: BIO-MEGA/BOEHRINGER INGELHEIM RESEARCH INC.
Laval Québec H7S 2G5 (CA)

(72) Inventors:
  • Anderson, Paul Cates
    Pierrefonds, Quebec, H8Y 3M8 (CA)
  • Moss, Neil
    Laval, Quebec, H7V 1B2 (CA)
  • Poupart, Marc-André
    Laval, Quebec, H7M 1B3 (CA)
  • Yoakim, Christiane
    Laval, Quebec, H7G 4T5 (CA)

(74) Representative: Laudien, Dieter, Dr. et al
Boehringer Ingelheim GmbH Abteilung Patente
D-55216 Ingelheim
D-55216 Ingelheim (DE)


(56) References cited: : 
   
       


    (54) HIV protease inhibitors containing derived amino acids


    (57) Disclosed herein are compounds of the general formula X-A-B-C'-Y wherein X is lower alkanoyl optionally substituted with one or two hydroxyls, A is an amino acid residue having a lower alkyl side chain, e.g. Ala or Val, B is a non-peptide linking unit, e.g. statyl or PheΨ[CH₂NH]Leu, C' is an amino acid residue of α-amino-β-cycloalkylpropionic acid, glutamic acid or α-aminoadipic acid, or a related derivative thereof, and Y is alkoxy, cycloalkoxy, a substituted alkoxy or a substituted amino group, e.g. cycloalkylalkoxy, arylalkoxy, alkylamino, (cycloalkyl)alkylamino or arylalkylamino. The compounds inhibit the activity of human immunodeficiency virus (HIV) protease and interfere with HIV induced cytopathogenic effects in human cells. These properties render the compounds useful for combating HIV infections.





    Search report